The AGC (PKA/PKG/PKC) family of serine-threonine kinases includes ROCK (Rho-associated protein kinase). Animals such as chicken, zebrafish, Xenopus, and mammals also have ROCKs (ROCK1 and ROCK2). With a molecular weight of 158 kDa, human ROCK1 is a significant RhoA small GTPase downstream effector. A kinase domain, an acoiled-coil region, and a Pleckstrin homology (PH) domain make up a mammalian ROCK. If RhoA-GTP is absent, the kinase activity of ROCKs is reduced by an autoinhibitory intramolecular fold. Since ROCK is a downstream effector protein of the small GTPase Rho, one of the primary regulators of the cytoskeleton, ROCK is involved in a variety of different cellular phenomena.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V35094 | CaMKP inhibitor sodium | 52789-62-5 | CaMKP inhibitor sodium is a selective ROCK1 inhibitor (antagonist) with IC50 of 14 nM. | |
V52297 | CAY10746 | 2247240-76-0 | CAY10746 is a selective Rho kinase (ROCK) inhibitor. | |
V53061 | Cotosudil | 1258833-31-6 | Cotosudil is a ROCK kinase inhibitor used in glaucoma or ocular hypertension research. | |
V55052 | Glycyl H-1152 hydrochloride | 913844-45-8 | Glycyl H-1152 HCl is a glycosyl analogue of the Rho-kinase inhibitor H-1152 di-HCl. | |
V2730 | GSK180736A | 817194-38-0 | GSK180736A (GSK-180736A) is a GRK2 inhibitor thatwasdeveloped as a novel and potent Rho-associated, coiled-coil-containing protein kinase (ROCK) inhibitor whichbinds to GRK2 (G protein-coupled receptor kinase 2) with IC50of 0.77 μM; G protein-coupled receptors (GPCRs) are central to many physiological processes. | |
V2561 | GSK269962 (GSK269962A) | 850664-21-0 | GSK269962 (also known as GSK269962A) is a novel, potent and selective inhibitor of ROCK (Rho-associated protein kinase) with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. | |
V3320 | GSK269962 HCl | 2095432-71-4 | GSK269962 HCl (also called GSK-269962A HCl),the hydrochloride salt ofGSK 269962A, is a selective ROCK (Rho-associated protein kinase) inhibitor with potential antihypertensive and cardioprotective activity. | |
V1345 | GSK429286A | 864082-47-3 | GSK429286A (also known as RHO15;GSK 429286A;RHO-15;GSK-429286A)is a potent, orally bioactive, andselective inhibitor of ROCK1/2 with antihypertensive effects. | |
V67533 | HA-100 dihydrochloride | 210297-47-5 | HA-100 di-HCl is a potent protein kinase inhibitor (antagonist) with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for PKG, PKA, PKC and MLC kinases respectively. | |
V52021 | HA-100 hydrochloride | 141543-63-7 | HA-100 HCl is a potent protein kinase inhibitor (antagonist) with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for PKG, PKA, PKC and MLC kinases, respectively. | |
V51967 | Hu7691 | 2360523-76-6 | Hu7691 is an orally bioactive, selective Akt inhibitor (antagonist) with IC50s of 4.0 nM, 97.5 nM and 28 nM for Akt1, Akt2 and Akt3 respectively. | |
V51966 | Hu7691 free base | 2241232-43-7 | Hu7691 free base is an orally bioactive, selective Akt inhibitor (antagonist) with IC50s of 4.0 nM, 97.5 nM and 28 nM for Akt1, Akt2 and Akt3 respectively. | |
V2563 | Kobe0065 | 436133-68-5 | Kobe0065 (Kobe 0065) is novel and potent inhibitor of the H-Ras-cRaf1 interaction whichexhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. | |
V2564 | PD0166285 | 185039-89-8 | PD0166285 (PD-0166285) is a novel and potent Wee1 and Chk1 inhibitor with anticancer activity and enzymatic activity at nanomolar concentrations (IC50s of 24 and 72 nM for WEE1 and Myt1, respectively). | |
V2562 | RK-33 | 1070773-09-9 | RK-33 is a potent and first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells. | |
V1346 | RKI-1447 | 1342278-01-6 | RKI-1447 (ROCK Inhibitor XIII; RKI 1447; RKI1447) is a potent small molecule inhibitor of ROCK1 and ROCK2 with potential antitumor activities againstbreast cancer. | |
V55726 | ROCK-IN-5 | 692870-25-0 | ROCK-IN-5 (compound IB-37) is a potent inhibitor of ROCK, ERK, GSK and AGC protein kinases. | |
V55727 | ROCK-IN-6 | 2489328-74-5 | ROCK-IN-6 is a potent ROCK2 inhibitor (antagonist) with IC50 of 2.19 nM. | |
V55725 | ROCK-IN-7 | 2376635-95-7 | ROCK-IN-7 (compound 9) is a ROCK kinase inhibitor. | |
V55724 | ROCK-IN-8 | 1621103-79-4 | ROCK-IN-8 (Example 4) is a ROCK inhibitor (antagonist) with IC50 of less than 100 nM. |